Search

Zinc is the second most valuable microelement after iron, according to its abundance in the human body. Supplementation of this metal is not straightforward because of several factors like phytates and interference of other minerals during gastrointestinal digestion. For the last several years, intensive research has been developing new forms of zinc supplements based on zinc‐binding peptides from food products. Except for the advantages of supplementation, zinc‐peptide complexes are expected to be drug candidates against various diseases. Zinc supplementation can be improved by protein hydrolysates and peptides due to their zinc‐binding ability. They enhance zinc supplementation and contribute to preventing conditions leading to zinc deficiency that cause various diseases. Research on food‐derived zinc‐binding peptides is progressing in two directions: the isolation and identification of individual peptides (1) and the preparation of zinc complexes of protein hydrolysates (2). Both approaches are primarily aimed at developing effective mineral supplements, although some work on the second approach is also related to nutrition and therapy. Because zinc–protein hydrolysate complexes are nonstandardized mixtures of peptides, their biological activity mechanisms can be difficult to study. Therefore, it is important to focus more research on the biological activity of individual zinc‐binding complexes and their zinc complexes. This work reviewed recent advances in isolating and identifying zinc‐binding peptides from food sources, preparing protein hydrolysate–zinc complexes, and their biological activities. The established sequences of zinc‐binding peptides have been compiled into a table to review their amino‐acid composition and sequence. We also highlighted approaches for isolating and determining the zinc‐binding capacity of peptides in this class. The structural features of peptides affecting their zinc‐binding property were discussed in one section. [ABSTRACT FROM AUTHOR]

Diabetic retinopathy (DR) is a specific microvascular problem of diabetes, which is mainly caused by hyperglycemia and may lead to rapid vision loss. Dietary polyphenols have been reported to decrease the risk of DR. Apocynum venetum L. leaves are rich in polyphenolic compounds and are popular worldwide for their health benefits as a national tea drink. Building on previous findings of antioxidant activity and aldose reductase inhibition of A. venetum, this study investigated the chemical composition of polyphenol-rich extract of A. venetum leaves (AVL) and its protective mechanism on ARPE-19 cells in hyperglycemia. Ninety-three compounds were identified from AVL by LC-MS/MS, including sixty-eight flavonoids, twenty-one organic acids, and four coumarins. AVL regulated the polyol pathway by decreasing the expression of aldose reductase and the content of sorbitol, enhancing the Na+K+-ATPase activity, and weakening intracellular oxidative stress effectively; it also could regulate the expression of autophagy-related proteins via the AMPK/mTOR/ULK1 signaling pathway to maintain intracellular homeostasis. AVL could restore the polyol pathway, inhibit oxidative stress, and maintain intracellular autophagy to protect cellular morphology and improve DR. The study reveals the phytochemical composition and protective mechanisms of AVL against DR, which could be developed as a functional food and/or candidate pharmaceutical, aiming for retina protection in diabetic retinopathy. [ABSTRACT FROM AUTHOR]

Background: Vitiligo is a complex disorder characterized by skin depigmentation; the canonical Wnt signaling pathway that involves β-catenin plays a crucial role in promoting the melanin production in melanocytes. Targeted inhibition of the Janus kinase JAK-STAT pathway can effectively diminish the secretion of the chemokine C-X-C motif ligand CXCL10, thereby safeguarding melanocytes. Ferula has been applied as a treatment regimen for a long period; however, its use for the treatment of vitiligo has not been previously documented. Methods: CCK-8 assay, Intracellular melanin content assay, Tyrosinase activity assay, Western blotting, qRT-PCR, and ELISA methods were employed. Using molecular docking verified the inhibitory effects of feshurin on the JAK1. Results: The sesquiterpene coumarin feshurin was separated from Ferula samarcandica. Feshurin was shown to induce GSK-3β phosphorylation, resulting in the translocation of β-catenin into the nucleus. This translocation subsequently upregulated the transcription of microphthalmia-associated transcription factor (MITF), leading to increased tyrosinase activity and melanin production. In addition, feshurin inhibited the production of chemokine CXCL10 via the JAK-STAT signaling pathway, which was verified by molecular docking. Conclusions: Based on these findings, it can be concluded that feshurin exhibits significant potential for the development of novel anti-vitiligo therapeutics. [ABSTRACT FROM AUTHOR]

Two undescribed pyrrolizidine alkaloids, 13-dehydrosenkirkine (1) and chloromethylretrorsine (2), along with three known analogues, onetine (3), retrorsine (4), and usaramine N-oxide (5), were isolated from Jacobaea vulgaris Gaertn. The structures of the undescribed compounds were elucidated by extensive spectrometric and spectroscopic techniques, including HRESIMS, NMR, calculated 13C-NMR DP4+ analysis and comparison with experimental and calculated ECD spectra. The undescribed compounds were evaluated for their antitumour activity against HT29, HeLa, and HepG2 cells. In addition, the intramolecular interactions and quadrupolar couplings were revealed by investigating the geometrical and electronic properties of three typical otonecine-type PAs in DFT theory. [ABSTRACT FROM AUTHOR]

Introduction: Artemisia absinthium L. is a well‐known medicinal, aromatic, and edible plant with important medicinal and economic properties and a long history of use in treating liver inflammation and other diseases; however, there has been insufficient progress in quality control. Objective: This study aimed to investigate the quality markers for the anti‐inflammatory and antioxidant activities of A. absinthium based on spectrum–effect relationship analysis. Materials and methods: Eighteen batches of A. absinthium from different origins were used. Chemical fingerprints were obtained by ultra‐performance liquid chromatography (UPLC). The chemical compositions were identified by quadrupole‐Orbitrap high‐resolution mass spectrometry. Anti‐inflammatory activity was assessed by inhibition of cyclooxygenase‐2 and 15‐lipoxygenase in vitro and inhibition of nitric oxide release in lipopolysaccharide‐induced BV‐2 cells. Antioxidant activity was assessed by DPPH and ABTS radical scavenging assays. The relationship between bioactivity and chemical fingerprints was then analyzed using chemometrics including gray relational analysis, bivariate correlation analysis, and orthogonal partial least squares analysis. Results: Different batches of A. absinthium extracts possessed significant anti‐inflammatory and antioxidant activities to varying degrees. Eighty compounds were identified from A. absinthium, and 12 main common peaks were obtained from the UPLC fingerprints. P3 (chlorogenic acid), P5 (isochlorogenic acid A), and P6 (isochlorogenic acid C) were screened as the most promising active compounds by correlation analysis and further validated for their remarkable anti‐inflammatory effects. Conclusion: This is the first study to screen the quality markers of A. absinthium by establishing the spectrum–effect relationship, which can provide a reference for the development of quality standards and further research on A. absinthium. The UPLC fingerprints of 18 batches of A. absinthium were established, and their anti‐inflammatory and antioxidant activities were investigated. The chemical compositions were identified. The active compounds were screened by spectrum‐effect relationship. Finally, chlorogenic acid, isochlorogenic acid A, and isochlorogenic acid C were screened as the main active compounds and validated experimentally. These compounds can be used as quality control markers for A. absinthium. This research provides a scientific basis and valuable reference for the quality control of A. absinthium. [ABSTRACT FROM AUTHOR]

Introduction: Mastic is a natural resin produced by Pistacia lentiscus L. (Anacardiaceae). The beneficial properties of this resin are attributed to its triterpenes and volatile compounds. Objective: This study was conducted to screen and characterize the terpenes in mastic ethyl acetate extract (M‐Ex). Methods: An ultrahigh‐performance liquid chromatography coupled to quadrupole Orbitrap high‐resolution mass spectrometry (UHPLC‐Q‐Orbitrap‐HRMS) method was developed for the qualitative analysis of terpenes in M‐Ex. We utilized in‐house‐isolated compounds as reference substance (Rs), including monoterpenes (A) with α‐pinane structures, tetracyclic triterpene (B) containing tirucallane skeletons, and pentacyclic triterpene (C) belonging to olean, moronic, amyrone, and lupane types. Based on the mass spectrometric characteristics of the above compounds, and the difference in characteristic diagnostic fragment ions (DFIs) in isomeric compounds, the terpene compounds were further identified in M‐Ex. Results: Out of a total of 70 compounds, including monoterpenes and tetra‐, and pentacyclic triterpenes, 20 were accurately determined by Rs, retention time (RT), and DFIs. Based on the cleavage patterns summarized from the above 20 compounds and with reference to the reported literature, another 50 compounds were putatively identified. Based on our discovery, six terpenic acids with A‐seco‐tirucallane types and one monoterpene dimer were identified for the first time in mastic. Conclusion: Our research serves not only as a foundation for the rapid identification and screening of terpene compounds in mastic but also as a supplementary basis for the identification of such compounds in other types of resins. Mastic (Pistacia lentiscus L.) is a natural resin. In this study, the terpenes in mastic ethyl acetate extract (M‐Ex) were qualitatively detected by UHPLC‐Q‐Orbitrap‐HRMS. A total of 70 compounds in M‐Ex were putatively identified based on the mass spectrometric characteristic of reference compounds (Rs) and the difference of characteristic diagnostic fragment ions (DFIs) in isomeric compounds. The result provides a basis for rapid identification and screening of terpene compounds in mastic and other types of resins. [ABSTRACT FROM AUTHOR]

Hepatitis B surface antigen (HBsAg) is not only the biomarker of hepatitis B virus (HBV) infection and expression activity in hepatocytes, but it also contributes to viral specific T cell exhaustion and HBV persistent infection. Therefore, anti-HBV therapies targeting HBsAg to achieve HBsAg loss are key approaches for an HBV functional cure. In this study, we found that YZH-106, a rupestonic acid derivative, inhibited HBsAg secretion and viral replication. Further investigation demonstrated that YZH-106 promoted the lysosomal degradation of viral L- and M-HBs proteins. A mechanistic study using Biacore and docking analysis revealed that YZH-106 bound directly to the PreS2 domain of L- and M-HBsAg, thereby blocking their entry into the endoplasmic reticulum (ER) and promoting their degradation in cytoplasm. Our work thereby provides the basis for the design of a novel compound therapy to target HBsAg against HBV infection. [ABSTRACT FROM AUTHOR]

This article discusses the isolation and structural elucidation of 17 flavonoids from the leaves and stems of Cassia nodosa, a plant used in traditional Chinese medicine. The compounds were identified using spectroscopic methods and compared with literature data. Some of the identified compounds include kaempferol, apigenin, velutin, quercetin, genkwanin, chrysoeriol, luteolin, kaempferol-3-O-α-L-rhamnoside, and kaempferitrin. Additionally, the document provides information on various compounds isolated from C. nodosa for the first time, including quercitrin, 2″,3″-diol acetonide-3-O-α-L-rhamnopyranoside-kaempferol, aromadendrin, engeletin, sakuranetin, naringenin, davidigenin, and 2,5-dimethyl-7-hydroxychromone. The research was supported by the Key Laboratory and Science and Technology Innovation Team of Higher Education in Yunnan, China. [Extracted from the article]

Over the past decades, increasing evidences have demonstrated that five retinoids, including retinol (ROL), retinol acetate (RAc), retinol propionate (RP), retinol palmitate (RPalm), and hydroxypinacolone retinoate (HPR), can be potential therapeutic agents for skin photoaging. However, therapeutic efficacies and biosafety have never been compared to these compounds. This study aimed to determine the optimal retinoid type(s) for anti‐photoaging therapy both in vitro and in vivo. Our data demonstrated that four retinoids (RPalm, RP, HPR and ROL) but not RAc were effective for anti‐photoaging treatment at 5 μg/mL in vitro, with action mechanisms associated with antioxidative, anti‐inflammatory and anti‐skin ECM degradation activities. Notably, both RPalm and RP appeared superior to HPR and ROL for those activities. Importantly, both RPalm and RP were shown to be optimal for anti‐photoaging therapy when topically applied at 5 mg/kg in a UVB‐induced mice model of photoaging, which is consistent with their high anti‐photoaging activities in vitro. Additionally, topical application of these five retinoids showed satisfactory biosafety without causing significant apoptosis in animal organs, although RP application led to a slight decline in animal body weights. Collectively, these data have laid a good foundation for the next development of the clinical application of these retinoids for skin healthcare. [ABSTRACT FROM AUTHOR]

Our research team has synthesized 33 tricyclic pyrazolopyrimidine arylidene ester derivatives using the lead compound CAM551 as a starting point. This was achieved by a designed five‐step synthesis strategy. The synthesized compounds' inhibitory activities against HT‐116 human colorectal adenocarcinoma cell line and HGC27 human gastric cancer cells were assessed through traditional MTT assays. The designed and synthesized compounds demonstrated superior inhibition against both types of cancer cells. Additionally, compound 7b, which contains a long‐chain substituent, exhibited improved inhibition against hepatocellular carcinoma cells and a greater safety profile. These findings indicate that compound 7b has the potential as an antitumor lead compound for future research. [ABSTRACT FROM AUTHOR]

This article discusses the chemical composition of compounds found in the leaves and stems of Erythrina crista-galli, a plant used in traditional medicine. The study conducted in Yunnan, China, identified alkaloids, flavonoids, isoflavonoids, coumestans, and pterocarpans with antimicrobial and phytoestrogenic activities. The chemical structures of the compounds were determined through spectroscopic analysis. This research provides valuable information for further exploration of the medicinal properties of Erythrina crista-galli. [Extracted from the article]

This article discusses the compounds found in the leaves and stems of the plant Cassia nodosa, which is widely distributed in several countries and used in traditional medicine. Previous studies have identified different types of compounds in the Cassia genus, but there are limited reports on C. nodosa specifically. In this study, 17 compounds were isolated and characterized, including anthraquinones, flavonoids, terpenoids, alkaloids, and steroids. The compounds were identified using spectroscopic methods and compared with existing literature data. The research was supported by the Key Laboratory and Science and Technology Innovation Team of Higher Education in Yunnan, China. [Extracted from the article]

Introduction: Fungal species are an attractive resource for physiologically functional food and drug precursor. Fomes officinalis Ames, a medicinal fungus, is traditionally used as a folk medicine in traditional Chinese medicine prescription for the therapy of cough and asthma. The water‐soluble substances in Chinese herbal medicines are likely to play an important physiological function. However, information on probing and identifying chemical components of the aqueous extract of Fomes officinalis Ames (AFO) remains unknown. Objective: This study was conducted to screen and characterise the chemical components of AFO. Material and Methods: An effective and sensitive ultrahigh‐performance liquid chromatography tandem quadrupole‐Orbitrap high‐resolution mass spectrometry (UHPLC‐Q‐Orbitrap‐HRMS) method with the Full MS/PIL/dd‐MS2 acquisition approach was applied for the profiling of chemical components in AFO. An HSS T3 column was used for component separation, and a strategy of simultaneous targeted and untargeted multicomponent characterisation was implemented. Multiple identification approaches were used, including accurate molecular mass and elemental composition matching, literature and database searching, and fragmentation rules elucidation. Results: A total of 115 components, including 20 amino acids and derivatives, six nucleobases, nine nucleosides, 75 dipeptides, two tripeptides, and three other components, were tentatively identified. Among them, the targeted exploring method screened six nucleobases and nine nucleosides including modified nucleosides. To our best knowledge, this is the first time a report has been done on the presence of the 115 compounds in AFO. Conclusion: Profiling and characterisation compounds of AFO enriched its material basis, which would lay the foundation for improving potential medicinal and nutritional values and effecting comprehensive quality control of Fomes officinalis Ames. The information on identifying the hydrophilic constituents of the aqueous extract of Fomes officinalis Ames was reported based on ultrahigh‐performance liquid chromatography tandem quadrupole‐Orbitrap high‐resolution mass spectrometry. Meanwhile, a comprehensive approach that consists of targeted and untargeted analytical strategy, database searching, and fragmentation rules elucidation was used to characterize the chemical composition. In total, 115 components, including 20 amino acids and derivatives, 6 nucleobases, 9 nucleosides, 75 dipeptides, 2 tripeptides, and 3 other components, were tentatively identified. [ABSTRACT FROM AUTHOR]

Two novel sesquiterpenes and one new monoterpene, together with eight reported compounds were isolated from dichloromethane–soluble extract of the aerial part of Artemisia tournefortiana Reichb. Their relative and absolute structures were elucidated based on the analysis of 1D and 2D NMR spectra, HRESIMS, and calculated electronic circular dichroism (ECD). Two sesquiterpenes (1 and 2) showed no inhibition effect in anti-inflammatory and cytotoxic activity tests. Three new terpenes (1–3) were tested for antibacterial activity, compounds 2 and 3 showed moderate antibacterial activities with minimum inhibitory concentrations (MICs) between 264 and 556 μg/ml. [ABSTRACT FROM AUTHOR]

Dichloromethane and butanol extracts of the roots of Prangos pabularia were analyzed to determine chemical constituents and biological activity. The new coumarin 1, yuganin B ((5-(((2S,3R,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-((2-oxo-2H-chromen-7-yl)oxy)tetrahydro-2H-pyran-3-yl)oxy)-3,4-dihydroxytetrahydrofuran-3-yl)methyl 4-hydroxy-3-methoxybenzoate) along with three phenolic and twenty-four known coumarins were isolated from the roots of Prangos pabularia, and the structures of these isolated compounds were elucidated by UV, HR-ESIMS, and 1 D and 2 D NMR spectroscopy. In addition, the anti-melanogenic effect of several of the isolated individual compounds and their inhibitory effect on B16 cells were evaluated. Isolating and testing compounds may proof to be useful in the treatment of hyperpigmentation and as a skin-whitening agent in the cosmetics industry. [ABSTRACT FROM AUTHOR]

An aurone derivative HJ-1, was isolated from Coreopsis tinctoria in our previous work, showed potential anti-hepatocellular carcinoma activity. From it, seventy-five compounds were synthesized via bioisostere and scaffold hopping strategy, and then submitted to the inhibitory activities evaluation against four tumor cells (HELA, HT-29, A549 and HepG2) through MTT assays. These activities have been discussed in SAR. Based on the results, compounds, thirty compounds showed moderate to good antitumour activity. Among them, five compounds (A3: 3.41 ± 1.03 μM, E3: 5.11 ± 0.23 μM, E8: 4.14 ± 1.21 μM, F2: 5.40 ± 1.18 μM, F4: 7.37 ± 0.87 μM) had achieved a comparable efficiency to the positive control DOX (Doxorubicin) against HT-29 cell lines, Compound A3 and F4 were identified as potential leading compounds. [ABSTRACT FROM AUTHOR]

The fingerprint of Vernonia anthelmintica effective part (VAEP) from 15 different producing areas was established, followed by cluster analysis and principal component analysis. The relationship between the fingerprint and the melanogenesis‐promoting activity of VAEP was then analyzed using the grey correlation degree and the orthogonal partial least square method. The characteristic peaks reflecting the pharmacodynamic effect of VAEP were identified as vernodalin, 3,5‐O‐dicaffeoyl quinic acid (3,5‐diCQA), and butin. Based on the distribution characteristics of these components in plants from different habitats and the verification of results from the spectrum–effect relationship, vernodalin and 3,5‐diCQA can be used as characteristic components for quality control and pharmacodynamic assessment of V. anthelmintica products. This research establishes a theoretical foundation for planting areas and provides a scientific evaluation of the melanogenesis‐promoting effect of V. anthelmintica. [ABSTRACT FROM AUTHOR]

This article discusses the compounds found in the leaves and stems of Premna fohaiensis, a plant species mainly found in Southern China. The study is the first to report on the isolation and identification of compounds from P. fohaiensis. The researchers collected the plant material, extracted it, and used chromatographic techniques to isolate and purify the compounds. The structures of the compounds were determined through spectroscopic analysis. Some of the compounds identified include hinokinin, savinin, and 9,9'-dihydroxysesamin. The article also provides information on the chemical composition of various compounds isolated from the genus Premna, including 2α,3α-Dihydroxyolean-12-en-28-oic acid, Ursolic acid, Betulinic acid, and others. The research was supported by various organizations and foundations. [Extracted from the article]

This article discusses the isolation and characterization of 15 phenolic compounds from the leaves and stems of Caesalpinia enneaphylla, a plant used in Chinese traditional medicine. The compounds include flavonoids, lignans, coumarin, and simple aromatics. The chemical structures of these compounds were identified through spectroscopic analysis. This research contributes to the search for new bioactive metabolites from Caesalpinia enneaphylla and provides valuable information for further studies on the medicinal properties of this plant. The document provides information on various compounds isolated from C. enneaphylla, including their chemical formula, physical properties, and spectroscopic data. The research was supported by the Key Laboratory and Science and Technology Innovation Team of Higher Education in Yunnan, China. [Extracted from the article]

Two new polyamine alkaloids (bufonines A-B), together with four known alkaloids, bufotenidine (3), bufotenine (4), 1-(β-d-ribofuranosyl)-lH-1,2,4-triazone (5) and proline (6) were isolated from the Bufo viridis toad venom. Their structures were identified by UV, HR-ESI-MS, NMR spectral analyses, and comparison of theoretical and experimental ECD data. All compounds were tested in vitro cytotoxicity against three human cancer cell lines (HT-29, A549 and Hela). None of the compounds showed cytotoxicity towards all tested cell lines. To the best of our knowledge, this is the first report of alkaloid components from Bufo viridis toad venom. [ABSTRACT FROM AUTHOR]

Tryptic hydrolysates of protein fractions obtained by the Osborne method from chickpea (Cicer arietinum L.) seeds interacted with zinc ions and the results of chelation were monitored by the Energy Dispersive X-Ray (EDX) technique. The glutelin hydrolysate (GluHyd) reacted with zinc ions and depicted a relatively higher zinc content. For this reason, the zinc complex of the glutelin hydrolysate (GluHyd-Zn) was studied deeper, and 11 peptides were identified in its more zinc-containing second fraction obtained after gel filtration. The peptide HKERVQLHIIPTAVGK showed a relatively higher chelating capacity (57.86 ± 2.14%). According to the result of the ICP-OS analysis, 1 mg peptide could chelate 381.61 ± 133.39 µg zinc, and the molar ratio of peptide-zinc was about 1:4. Spectral methods proved that side chain and C-termini carboxyl groups of the peptide mostly were involved in chelation and N atoms of amino side chains, imidazole group of histidine, and N-termini at some extents were occupied by the metal ions. Modeling of zinc-peptide interaction was done using Molecular Operating Environment (MOE) software. The results of the docking correlate with the experimental data. ACE2 inhibitory effect of HKERVQLHIIPTAVGK-Zn complex (IC50 = 1.5 mg/mL) was better than that of HKERVQLHIIPTAVGK (IC50 = 2.2 mg/mL). [ABSTRACT FROM AUTHOR]

Bufadienolides, naturally found in toad venoms having steroid‐like structures, reveal antiproliferative effects at low doses. However, their application as anticancer drugs is strongly prevented by their Na+/K+‐ATPase binding activities. Although several kinds of research were dedicated to moderating their Na+/K+‐ATPase binding activity, still deeper fundamental knowledge is required to bring these findings into medical practice. In this work, we reviewed data related to anticancer activity of bufadienolides such as bufalin, arenobufagin, bufotalin, gamabufotalin, cinobufotalin, and cinobufagin and their derivatives. Bufotoxins, derivatives of bufadienolides containing polar molecules mainly belonging to argininyl residues, are reviewed as well. The established structures of bufotoxins have been compiled into a one‐page figure to review their structures. We also highlighted advances in the structure‐modification of the structure of compounds in this class. Drug delivery approaches to target these compounds to tumor cells were discussed in one section. The issues related to extraction, identification, and quantification are separated into another section. [ABSTRACT FROM AUTHOR]

A facile protocol was developed for the combinatorial synthesis of furo[2,3-d]pyrimidinone and pyrrolo[2,3-d]pyrimidinone library via a one-pot condensation, from 2-amino furans/pyrroles. Herein reported process required a similar reaction condition, providing mild access to two diverse series of natural product-like heterocycles. Both furo[2,3-d]pyrimidinones and pyrrolo[2,3-d]pyrimidinones were evaluated in vitro against a panel of human cancer cell lines including against human cancer HeLa (cervical), MCF-7 (breast) and HT-29 (colon) cell lines. Derivative 12n ((2-(4-chlorophenyl)-1-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrrolo[2,3-d]pyrimidin-4(1H)-one)) showed high activity (IC50 = 6.55 ± 0.31 µM) against the HeLa cell line. These products could be subjected to a various modification and therefore represent important skeletons for the anticancer drug discovery. [ABSTRACT FROM AUTHOR]

Vitiligo, an acquired depigmentation disorder, is characterized by the loss of functional melanocytes and epidermal melanin. In recent years, research has focused on promoting melanin biosynthesis and protecting melanocytes to reduce stress-related damage for the purpose of applying it to vitiligo treatment. Ruta graveolens L. has been utilized as a medicinal herb in diverse traditional medicine systems to address conditions like vitiligo. In this investigation, we isolated and purified 16 unique alkaloid compounds from the chloroform extracts of R. graveolens, encompassing a new quinoline alkaloid and several recognized compounds. Bioactivity analysis showed that compound 13, an alkaloid derived from R. graveolens, promotes melanin production while protecting PIG3V melanocytes against 4-tert-butylphenol (4-TBP)-induced oxidative damage by downregulating endoplasmic reticulum (ER) stress and pro-inflammatory cytokines through interleukin-6 (IL-6) regulation. Additionally, the compound suppressed the expression of Bip, IRE1, p-IRE1, and XBP-1 proteins, suggesting a potential antioxidant function. These findings suggest that compound 13 isolated from R. graveolens can augment melanogenesis in melanocytes, reduce endoplasmic reticulum (ER) stress, and ameliorate vitiligo exacerbation. The melanogenic activity observed in the chloroform fraction emphasizes R. graveolens's potential as a novel therapeutic target for vitiligo treatment, warranting further exploration in future studies. [ABSTRACT FROM AUTHOR]

Background: Xuelian granule (XL), a traditional Chinese medicine (TCM) formula, has been used for the treatment of diabetic nephropathy for a long time as a hospital preparation. Because the active ingredients in the XL that can help to treat diabetic nephropathy are still unclear, which limits the interpretation for its pharmacological mechanism, further development and subsequent study on the material basis of its efficacy. Methods: In this study, a screening method based on inhibition activity against aldose reductase (AR) was employed for activity-directed chemical analysis of XL using ultra-high performance liquid chromatography combined with quadrupole-orbitrap high resolution mass spectrometry (UHPLC-Q-orbitrap-HRMS) technique. Results: A total of 178 compounds, including 46 terpenes, 47 organic acids, 25 flavonoids, 29 phenylethanoid glycosides, and 31 other types, were tentatively identified from XL which might responsible for its AR inhibition activity. Conclusion: This is the first study for a systematic, rapid, and accurate qualitative analysis of XL. This research provides a scientific and experimental basis for further researches on pharmacodynamics material basis and quality control of XL. [ABSTRACT FROM AUTHOR]

Dracocephalum Moldavica L. is a traditional herb for improving pharynx and relieving cough. However, the effect on pulmonary fibrosis is not clear. In this study, we explored the impact and molecular mechanism of total flavonoid extract from Dracocephalum moldavica L. (TFDM) on bleomycin‐induced pulmonary fibrosis mouse model. Lung function testing, lung inflammation and fibrosis, and the related factors were detected by the lung function analysis system, HE and Masson staining, ELISA, respectively. The expression of proteins was studied through Western Blot, immunohistochemistry, and immunofluorescence while the expression of genes was analyzed by RT‐PCR. The results showed that TFDM significantly improved lung function in mice, reduced the content of inflammatory factors, thereby reducing the inflammation. It was found that expression of collagen type I, fibronectin, and α‐smooth muscle actin was significantly decreased by TFDM. The results further showed that TFDM interferes with hedgehog signaling pathway by decreasing the expression of Shh, Ptch1, and SMO proteins and thereby inhibiting the generation of downstream target gene Gli1 and thus improving pulmonary fibrosis. Conclusively, these findings suggest that TFDM improve pulmonary fibrosis by reducing inflammation and inhibition of the hedgehog signaling pathway. [ABSTRACT FROM AUTHOR]

A new unsaturated fatty glycoside Humionoactosides A, together with four known compounds were isolated from the whole plant of Euphorbia humifusa Willd. Their structures were identified by MS/MS, NMR and ECD spectroscopic analyses, and comparison with the literature data. All compounds were evaluated for the effect on melanogenesis and tyrosinase activity use B16 cells in vitro, and the results showed that compound 1 could significantly improve the formation of melanin (138.7%, 50 μM) and tyrosinase activity (137.2%, 50 μM) compared with the positive control 8-MOP (125.2%, 138.9%, 50 μM) in a dose-dependent manner. This is the first time that those compounds reported from Euphorbia humifusa Willd. with potential anti-vitiligo activity. [ABSTRACT FROM AUTHOR]

Hyssopus cuspidatus Boriss. grows in Xinjiang, China. A new macrocyclic spermidine alkaloid, namely hyssopusizine (1), along with sixteen known compounds were isolated and identified from the aerial parts of H. cuspidatus. Their structures were elucidated on the basis of spectroscopic data and comparison with the literature. Among them, fifteen compounds were isolated from H. cuspidatus for the first time. The absolute configuration of compound 1 was established by comparing the calculated and experimental ECD spectroscopic data. All isolated compounds were tested for their antioxidant and antimicrobial activities. Among them, compound 10 exhibited significant effects on ABTS free-radical scavenging activity with an IC50 value of 15.6 μM. Compounds 5–7 exhibited potent antioxidant activities against ABTS and DPPH. Most compounds exhibited moderate antimicrobial activities. Hyssopusizine (1) is the first macrocyclic spermidine alkaloid discovered from the Hyssopus genus. [ABSTRACT FROM AUTHOR]

Given the limitations of existing antiviral drugs and vaccines, there is still an urgent need for new anti-influenza drugs. CAM106, a rupestonic acid derivative, was studied for its potent antiviral activity and showed a favorable inhibitory effect on influenza virus replication. However, many gaps exist in preclinical studies of CAM106. This study focused on the pharmacokinetic profile and metabolites of CAM106 in vivo. An efficient and fast bioanalytical method was successfully developed and validated for the quantitation of CAM106 in rat plasma. A mobile phase aqueous solution (A, containing 0.1% formic acid) and acetonitrile (B) worked within 0–3.5 min, with 60% B. The mass spectrum scanning mode was the parallel reaction monitoring (PRM) with a resolution of 17,500. The linear range of the method was 2.13–1063.83 ng/mL. The validated method was applied to a pharmacokinetic study in rats. The matrix effects ranged from 93.99% to 100.08% and the recovery ranged from 86.72% to 92.87%. The intra- and inter-day precisions were less than 10.24% and the relative error (RE) ranged from −8.92% to 7.1%. The oral bioavailability of CAM106 was 1.6%. Thereafter, its metabolites in rats were characterized using high-resolution mass spectrometry. The isomers M7-A, M7-B, M7-C, and M7-D were well separated. As a result, a total of 11 metabolites were identified in the feces, urine, and plasma of rats. The main metabolic pathways of CAM106 were oxidation, reduction, desaturation, and methylation. The assay was reliable and provided useful information for further clinical studies of CAM106. [ABSTRACT FROM AUTHOR]

Bufadienolides, cyclopentanophenantrene derivatives that possess similar structures to cardiac glycosides, have been established to reveal cytotoxicity. Their higher concentrations as anticancer means are expected to affect the normal function of the heart, liver, and kidney. In this work, we established the mass ratio of bufadienolides isolated from the venom of Bufo viridis. Arenobufagin, gamabufotalin, telocinobufagin, and marinobufagin were found as the major compounds in the sum. Their effects on biological parameters, used as indicators of the normal functioning of organs, were determined in rabbits. The blood samples, taken on the 10th and 30th days following the drug administration, showed these paramaters reaching the control levels for 30 days in all studied doses: 0.15, 0.45, and 0.6 mg/kg. The 0.15 and 0.6 mg/kg doses were established not to cause significant changes in the activities of alanine aminotransferase and aspartate aminotransferase, and the quantities of cholesterol and fasting blood sugar in blood samples. Significant changes were found in quantities of glucose (a reduction) and urea (an increase) on the 10th day of the administration. But their levels reached the control level for the next 20 days. We observed significant differences in thromboelastographic parameters in mice on the 10th day after the drug administration in a 0.15 mg/kg dose. In mice, LD50 levels of intravenous, subcutaneous, and oral administrations made 14.5, 110, and 215 mg/kg, respectively. These results enable the suggestion of optimum concentration that does not cause severe damage to the functions of organs. [ABSTRACT FROM AUTHOR]

Acetaminophen (N-acetyl-p-aminophenol, APAP) is regularly used for antipyretic and analgesic purposes. Overdose or long-term exposure to APAP could lead to liver damage and hepatotoxicity. In this study, the approach of enhanced electrochemical detection of APAP by nanostructured biomass carbon/silver was developed. Porous biomass carbon derived from Elaeagnus Angustifolia gum was prepared by pyrolysis with co-doping of electron-rich elements of nitrogen, sulfur, and phosphorus. The electrodeposition of silver onto a glassy carbon electrode modified with porous carbon could enhance the sensing signal towards APAP. Two linear ranges from 61 nM to 500 μM were achieved with a limit of detection of 33 nM. The developed GCE sensor has good anti-interference, stability, reproducibility, and human urine sample analysis performance. The silver-enhanced biomass carbon GCE sensor extends the application of biomass carbon, and its facile preparation approach could be used in constructing disposable sensing chips in the future. [ABSTRACT FROM AUTHOR]

Aflatoxin determination is imperative among agricultural and food products as the pollution of the toxic aflatoxin could cause severe hazards towards animals and human beings. Here, we prepared Elaeagnus gum derived porous carbon material as electrode modified material. In situ electropolymerization of molecularly imprinted polymer utilizing phenol as monomer and aflatoxin B1 as target template was further processed onto the porous carbon surface to achieve aflatoxin B1 sensing ability. This sensitive MIP sensor has a detection range from 5 pM to 100 pM of aflatoxin B1, an electrochemical sensitivity of 82.4 μA log(pM)−1 cm−2 with a detection limit of 1.7 pM, and a recovery rate of real sample measurement is 98.21 %. Good selectivity, fair repeatability and stability was confirmed. This work demonstrates the promising application of Elaeagnus gum derived porous carbon modified electrode sensor for food and drug monitoring. [ABSTRACT FROM AUTHOR]

Nineteen compounds, including seventeen alkaloids O-methylarmepavine (1), (S)-6-methoxy-1-(4-methoxybenzyl)-2-methyl -1,2,3,4-tetrahydroisoquinolin-7-ol (2), (+)-(IR,laR)-lahydroxymagnocurarin (3), (6R,6aS,P)-(+)-corydine (4), (+)-N-methyllaurotetanine (5), magnoflorine (6), 3-hydroxy-1,2-dimethoxy-5-methyl-5H-dibenzoindol-4-one (7), imperialine (8), crispine B (9), (S)-1-(3-methoxyphenyl)-N-methylpropan-2-amine (10), methyl 2- (acetamino)benzoate (11), 2-carboxyoxanilic acid methylester (12), 4-[2-(methoxycarbonyl) anilino]-4-oxobutanoic acid methyl ester (13), N-methylcorydaldine (14), N-methyl-6,7- dimethoxyisoquinolone (15), (5S,6R,7S,8R)-5-amino-(2Z,4Z)-1,2,3-trihybuta-2,4-dienyloxypentane- 6,7,8,9-tetraol (16), nicotinic acid (17), and two megastigmane type compounds, S(+)- dehydrovomifoliol (18) and megastigmane (19), were isolated from the Aconitum barbatum var. puberulum Ledeb. Compounds 1–3 and 5–19 were isolated from this plant for the first time, of which compound 11 was isolated from natural source for the first time. Cytotoxicity evaluation revealed that compound 5 displayed mild cytotoxicity against the Hela cell lines (IC50 13.69 ± 0.036 μM). Antibacterial activity evaluation revealed that compounds 1 and 6 showed strong antibacterial activity against the Gram-positive bacterium, S. aureus. [ABSTRACT FROM AUTHOR]

An integrated strategy was developed for the systematic chemical fingerprint and chemometrics analysis for the quality assessment of Aloe vera (L.) Burm. f. The ultra-performance liquid chromatography fingerprint was established, and all common peaks were tentatively identified by using ultra-high-performance liquid chromatography hyphenated with quadrupole–orbitrap-high-resolution mass spectrometry. Afterwards, the datasets of common peaks were subjected to hierarchical cluster analysis, principal component analysis and partial least squares discriminant analysis to holistically compare the differences. The results revealed that the samples were predicted to fall into four clusters, which were related to four different geographical locations. Using the proposed strategy, aloesin, aloin A, aloin B, aloeresin D and 7-O-methylaloeresin A were rapidly determined to be the potential characteristic quality markers. Finally, five screened compounds in 20 batches of samples were simultaneously quantified, and their total contents were ranked as follows: Sichuan province > Hainan province > Guangdong province > Guangxi province, which suggests that geographical origins may be an important factor affecting the quality of A. vera (L.) Burm. f. This new strategy can not only be used to explore possibly the latent active substance candidates for pharmacodynamic studies, but it is also an efficient analytical strategy for other complex traditional Chinese medicine systems. [ABSTRACT FROM AUTHOR]

Herein, we studied the formation of thiones via C=O group conversion into the C=S functional group-based tricyclic pyrimidinone systems using Lawesson's reagent and phosphorus pentasulfide as thionation agents. Naturally occurring alkaloids deoxyvasicinone and mackinazolinone were selected as templates for the modification of furo[2,3-d]pyrimidinone and pyrrolo[2,3-d]pyrimidinone scaffold. Research work was performed under the combinatorial and parallel synthesis of pyrimidine-based small molecules, along with a one-pot reaction strategy. All synthesized 54 novel pyrimidine-thiones were elucidated by 1H-NMR, 13C-NMR, and HRMS analysis. In addition, both series of thiones were evaluated for their antitumor activity against three types of the human cancer cell: cervical HeLa, breast MCF-7, and colon HT-29 lines. Compound with azepine fragment 13aa (1-methyl-2-(4-(trifluoromethyl)phenyl)-1,6,7,8,9,10-hexahydro-4H-pyrrolo[2',3':4,5]pyrimido[1,2-a]azepine-4-thione) was most active derivative (IC50 = 2.09 ± 0.22 µM) against the HT-29 cell line. [ABSTRACT FROM AUTHOR]

Three new feruloyl glucuronopyranosyl glycerols, 1-O-α-D-(2′-feruloyl) glucuronopyranosyl glycerol (1), 1-O-α-D-(3′-feruloyl) glucuronopyranosyl glycerol (2), and 1-O-α-D-(4′-feruloyl) glucuronopyranosyl glycerol (3) were isolated and purified from the capitulum of Eriocaulon buergerianum Koern. Their structures were identified by spectroscopic and chemical methods. Molecular docking study showed that 1 is a potential inhibitor of TGF-β1 receptor. Bioassay results revealed that 1 exhibited strong inhibitory activity against the TGF-β-induced expression of α-smooth muscle actin (α-SMA) and fibronectin in human hepatic stellate LX-2 cells. The results in this study indicated that the new feruloyl glucuronopyranosyl glycerol 1 has preventive and therapeutic potentials against hepatic fibrosis. [ABSTRACT FROM AUTHOR]

Quercetin 3-O-(6″-O-E-caffeoyl)-β-D-glucopyranoside is a flavonoid compound produced by various plants with reported antiprotozoal potential against E. histolytica and G. lamblia; however, its effects on skin pigment regulation have not been studied in detail. In this investigation, we discovered that quercetin 3-O-(6″-O-E-caffeoyl)—D-glucopyranoside (coded as CC7) demonstrated a more increased melanogenesis effect in B16 cells. CC7 exhibited no cytotoxicity or effective stimulating melanin content or intracellular tyrosinase activity. This melanogenic-promoting effect was accompanied by activated expression levels of microphthalmia-associated transcription factor (MITF), a key melanogenic regulatory factor, melanogenic enzymes, and tyrosinase (TYR) and tyrosinase-related protein-1 (TRP-1) and 2 (TRP-2) in the CC7-treated cells. Mechanistically, we found that CC7 exerted melanogenic effects by upregulating the phosphorylation of stress-regulated protein kinase (p38) and c-Jun N-terminal kinase (JNK). Moreover, the CC7 upregulation of phosphor-protein kinase B (Akt) and Glycogen synthase kinase-3 beta (GSK-3β) increased the content of β-catenin in the cell cytoplasm, and subsequently, it translocated into the nucleus, resulting in melanogenesis. Specific inhibitors of P38, JNK, and Akt validated that CC7 promotes melanin synthesis and tyrosinase activity by regulating the GSK3β/β-catenin signaling pathways. Our results support that the CC7 regulation of melanogenesis involves MAPKs and Akt/GSK3β/β-catenin signaling pathways. [ABSTRACT FROM AUTHOR]

Fraction C SB 6 sb (2.98 g) was subjected to repeated silica gel column, eluting with petroleum ether- Me SB 2 sb CO (10:1->1:1), and then purified by Sephadex LH-20 column with CHCl SB 3 sb -MeOH (3:2), to produce B 2 b (10.0 mg), B 5 b (4.0 mg), B 6 b (5.5 mg), and B 8 b (3.6 mg). Fraction C SB 5 sb (0.56 g) was subjected to repeated silica gel column, eluting with petroleum ether-Me SB 2 sb CO (15:1->1:1), and then purified by Sephadex LH-20 column with CHCl SB 3 sb -MeOH (3:2) to obtain B 3 b (15.0 mg), B 4 b (7.5 mg), and B 7 b (10.6 mg). Fraction C4 (3.1 g) was separated by silica gel column with petroleum ether-Me SB 2 sb CO (20:1), and then on Sephadex LH-20 with CHCl SB 3 sb -MeOH (3:2), to yield B 9 b (16.5 mg), and B 10 b (4.2 mg). Fraction C3 (1.5 g) was isolated on Sephadex LH-20 with CHCl SB 3 sb -MeOH (3:2), and then purified on a silica gel column with petroleum ether-Me SB 2 sb CO (20:1) to afford B 1 b (20.1 mg) and B 11 b (30.5 mg). [Extracted from the article]

Carum carvi L. belongs to the Apiaceae family and is widely used as a vegetable, food spice, preservative, and herbal medicine. This study investigated the impact of essential oil extracted from Carum carvi L. seeds (CEO) on methicillin-resistant Staphylococcus aureus (MRSA) and its possible action mechanism. The dominant chemical components of CEO determined by GC-MS were carvone and limonene. It was observed that CEO had a considerable inhibitory effect against the growth of planktonic bacteria and biofilm in MRSA cells. Untargeted metabolomics based on GC-Q-TOF-MS was used to analyze the possible mechanism of the interaction of MRSA with CEO. It was determined that there were 63 different metabolites based on fold change values greater than 1.5 or less than 1.5, p < 0.05, VIP > 1, which demonstrated amino acid metabolism in MRSA was significantly affected by CEO. In conclusion, CEO has a potent antimicrobial property and has promising potential for use in food and drugs. [ABSTRACT FROM AUTHOR]

The EtOAc extract (70 g) was subjected to CC (silica gel, petroleum ether-EtOAc, 50:1->0:1), to afford seven fractions on the basis of TLC analysis, whereby fraction 2 (3 g) was separated on Sephadex LH-20 with CHCl SB 3 sb -MeOH (3:2) to get two subfractions (2.1-2.2). Fraction 5 (5.5 g) was separated on Sephadex LH-20 with CHCl SB 3 sb -MeOH (3:2), silica gel column with petroleum ether-EtOAc (20:1->0:1), and then further purified by semipreparative HPLC (Eclipse XDB-C SB 18 sb column, 9.4 × 250 mm, 5 m, flow rate 3 mL/min, UV 254 nm) with CH SB 3 sb OH-H SB 2 sb O (65:35) to yield B 5 b (6 mg), B 10 b (4.3 mg), and B 11 b (3.0 mg). Subfraction 4.2 (2.7 g) was separated on a silica gel column using a gradient solvent petroleum ether-EtOAc (20:1->0:1) to obtain six subfractions (4.2.1-4.2.6). Fraction 6 (5.9 g) was subjected to silica gel column, eluting with petroleum ether-EtOAc (15:1->0:1), and then purified by semipreparative HPLC with CH SB 3 sb OH-H SB 2 sb O (55:45) to yield B 3 b (4.5 mg), B 4 b (3.5 mg), and B 6 b (8 mg). [Extracted from the article]

As one of the prominent medicinal plants listed in the Chinese pharmacopoeia (2020), Saussurea involucrata (Kar. et Kir.) Sch.-Bip was demonstrated to possess various therapeutic effects. In our recent research, we extracted the polysaccharides from S. involucrata (SIP) at optimal conditions and conducted further structure elucidation on the main fraction as well as the confirmation of its possible anti-inflammatory activity. Hence, in this work, we assessed the in vitro antioxidant activity and anti-melanogenesis effects of the crude SIP in forskolin-induced B16F10 melanoma cells. The results show that SIP possessed strong antioxidant activity and was effective in concentration-dependently decreasing melanin formation and inhibiting tyrosinase activity in forskolin-induced B16F10 cells. Based on these results, the inhibitory mechanism of melanogenesis was investigated by measuring Tyrosinase (TYR), Tyrosinase related protein-1 (TRP-1), Tyrosinase related protein-2 (TRP-2), Microphthalmia-associated transcription factor (MITF), cAMP-response element binding protein (CREB), mitogen-activated protein kinases (MAPK) signaling protein members, and β-catenin degradation in forskolin-induced B16F10 cells. The anti-melanogenesis response of SIP might be attributed to the regulation of c-Jun N-terminal kinase (JNK) phosphorylation and β-catenin degradation pathways. These results suggest that polysaccharides from S. involucrata possess a strong anti-melanogenic effect, and thus could be used as a high-value natural material for skin whitening in cosmeceutical industries. [ABSTRACT FROM AUTHOR]

Polyphenols, a class of bioactive compounds existing in food and fruit, play an essential role in anti‐oxidation, anti‐inflammation, anticancer, anti‐atherosclerosis, and antiaging by scavenging free radicals, regulating cellular redox potential, signaling pathways, and so on. Due to the low bioavailability/high activity paradox, the functional mechanism of polyphenols in biomedicine has attracted widespread attention. This review summarizes polyphenols (especially quercetin) chemical structure and bioactive mechanism (signaling pathways, enzyme activity, cell redox potential, and gene expression) to show in‐depth biomedical functional mechanisms for the control of chronic heath diseases such as oxidation, inflammation, cancer, atherosclerosis, and aging. This study can deepen the understanding of polyphenols' effects on human health. Novelty impact statement: Providing another perspective for the comprehensive reuse of polyphenols in food and fruit.Summarizing the polyphenols in biomedical research progress of function mechanism.Deeping the understanding of the effects of polyphenols on human health. [ABSTRACT FROM AUTHOR]

This study aimed to investigate the anti‐inflammatory activity of Prunus cerasifera Ehrhart (EHP). LC–MS/MS, network pharmacology, enzyme‐linked immunosorbent assay (ELISA), and Western blot analysis methods were used to investigate the chemical composition and the anti‐inflammatory mechanism of EHP. The LC–MS/MS results showed that flavonoids and phenolic acids were the major compounds in EHP. The network pharmacology analysis results indicated that EHP was related to TNF, inflammatory cytokine, and MAPK signaling pathway. ELISA and Western blot results showed that EHP impeded the increase in inflammatory factors, inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX‐2), nuclear transcription factors κB (p65), MAPK pathway, pyrolytic relevant proteins nod‐like receptor family pyrin domain‐containing 3 (NLRP3), and interleukin‐1β (IL‐1β) induced by lipopolysaccharide (LPS) and activated the nuclear factor erythroid 2‐related factor 2 (Nrf2)/hemeoxygenase‐1 (HO‐1) pathway. Therefore, this research highlighted the potential application of P. cerasifera in the development of anti‐inflammatory foods that prevented inflammatory diseases. Practical applications: In recent years, many synthetic drugs with anti‐inflammatory effect have the disadvantages of high price and side effects. Thus, the development of anti‐inflammatory drugs from natural resources has its application value. In this study, LPS‐stimulated RAW264.7 cells were used to establish inflammatory model to verify the anti‐inflammatory effect of Prunus cerasifera (EHP). The results showed that P. cerasifera possessed anti‐inflammatory activity through inhibiting pro‐inflammatory cytokines secretion, NF‐κB, MAPK pathway, and NLRP3 inflammasome activation. Therefore, P. cerasifera has the potential to develop into functional food to prevent the progress of various inflammatory‐related diseases. [ABSTRACT FROM AUTHOR]

Psoralen, a major furocoumarin component of the Fructus Psoralen (FP), in combination with ultraviolet radiation, cures abnormal pigmentation disorder. In a previous study, we synthesized a series of linear furocoumarins with different substituents, out of which 5-((diethylamino)methyl)-3-phenyl-7H-furo [3,2-g] chromen-7-one (encoded as 5D3PC) showed better pigmenting effect than others in B16 cells. In this study, we examined the mechanism underlying the melanogenic effect of 5D3PC both in vivo and in vitro. To examine the pigmentation effect, the B16 and human melanocyte cell lines, PIG1 and PIG3V melanocytes were incubated with 5D3PC. In animal experiments, C57BL/6 mice received 5% hydroquinone and were administrated with 5D3PC for 30 days. 5D3PC upregulated the melanin synthesis and tyrosinase in B16 cell, PIG1 and PIG3V. The expression level of tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1) and tyrosinase-related protein-2 (TRP-2), microphthalmia-associated transcription factor (MITF), cyclic adenosine monophosphate (cAMP), phosphorylation of cAMP-responsive element binding protein (p-CREB), phosphorylation of p38 mitogen-activated protein kinase (MAPK), c- phosphorylation of Jun N-terminal kinase (p-JNK) was significantly higher in 5D3PC-treated B16 cells. The oral administration of 5D3PC attenuated the depigmentation of the C57BL/6 vitiligo mice model by increasing the numbers of melanin-containing hair follicles, melanogenic protein, and melanogenesis-relative genes expression in skin tissues. [ABSTRACT FROM AUTHOR]

The flora of Kazakhstan is characterized by its wide variety of different types of medicinal plants, many of which can be used on an industrial scale. The Traditional Kazakh Medicine (TKM) was developed during centuries based on the six elements of ancient Kazakh theory, associating different fields such as pharmacology, anatomy, pathology, immunology and food nursing as well as disease prevention. The endemic Artemisia L. species are potential sources of unique and new natural products and new chemical structures, displaying diverse bioactivities and leading to the development of safe and effective phytomedicines against prevailing diseases in Kazakhstan and the Central Asia region. This review provides an overview of Artemisia species from Central Asia, particularly traditional uses in folk medicine and the recent numerous phytochemical and pharmacological studies. The review is done by the methods of literature searches in well-known scientific websites (Scifinder and Pubmed) and data collection in university libraries. Furthermore, our aim is to search for promising and potentially active Artemisia species candidates, encouraging us to analyze Protein Tyrosine Phosphatase 1B (PTP1B), α-glucosidase and bacterial neuraminidase (BNA) inhibition as well as the antioxidant potentials of Artemisia plant extracts, in which endemic species have not been explored for their secondary metabolites and biological activities so far. The main result of the study was that, for the first time, the species Artemisia scopiformis Ledeb. Artemisia albicerata Krasch., Artemisia transiliensis Poljakov, Artemisia schrenkiana Ledeb., Artemisia nitrosa Weber and Artemisia albida Willd. ex Ledeb. due to their special metabolites, showed a high potential for α-glucosidase, PTP1B and BNA inhibition, which is associated with diabetes, obesity and bacterial infections. In addition, we revealed that the methanol extracts of Artemisia were a potent source of polyphenolic compounds. The total polyphenolic contents of Artemisia extracts were correlated with antioxidant potential and varied according to plant origin, the solvent of extraction and the analytical method used. Consequently, oxidative stress caused by reactive oxygen species (ROS) may be managed by the dietary intake of current Artemisia species. The antioxidant potentials of the species A. schrenkiana, A. scopaeformis, A. transiliensis and Artemisia scoparia Waldst. & Kitam. were also promising. In conclusion, the examination of details between different Artemisia species in our research has shown that plant materials are good as an antioxidant and eznyme inhibitory functional natural source. [ABSTRACT FROM AUTHOR]

Caraway, a well‐known traditional Uyghur medicine, has been used to treat vitiligo for centuries. Its biological effects on melanin synthesis of caraway have been investigated. However, beyond psoralen and isopsoralen alone, no further chemical component of caraway has been revealed. In this study, ultra‐high performance liquid chromatography coupled with hybrid quadrupole orbitrap mass spectrometry was employed to comprehensively characterize the chemical components present in caraway. Based on accurate mass measurements, key fragmental ions and comparison with reference standards, 75 chemical components were identified in caraway. Moreover, a tandem mass spectrometry method was developed and validated for quantitative analysis of three pairs isomeric components, namely psoralen/isopsoralen, bavachin/isobavachalcone and bavachromene/isobavachromene in rat plasma. Psoralen, isopsoralen, bavachin, and isobavachalcone showed linearity with concentration ranging of 1.0–500.0 ng/ml. The linear ranges for bavachromene and isobavachromene were 0.2–500.0 ng/ml. The accuracies were in ranges of 85%–115% with coefficient of variation errors of less than 15%. Furthermore, the method was applied to quantify the three pairs isomeric components in rats after oral administration of caraway. [ABSTRACT FROM AUTHOR]

A series of aurone compounds with the B ring substituted by different heterocycles has been synthesized. All synthesized compounds have been tested for antibacterial activity. It has been determined that different heterocyclic substituents modulate the antibacterial spectrum of aurones. Indole-substituted aurones display good inhibitory activity against Gram-positive bacteria. Thiophene-substituted aurones exhibit inhibitory activity against fungi. Aminopyrimidine-substituted aurones exhibit promising inhibitory activity against Gram-negative bacteria. We have determined that 2-arylimidazo[1,2-a]pyridones can be used as a platform for antifungal agents design. [ABSTRACT FROM AUTHOR]